JP7310149B2 - oral composition - Google Patents

Description

TECHNICAL FIELD The present invention relates to an oral composition that reduces irritation to the oral mucosa and provides a high feeling of warmth and coolness that lasts after use.

Oral compositions are blended with sensation-imparting ingredients such as hot pepper extracts and other cooling sensation-imparting ingredients, such as menthol, to impart warmth and cooling sensations, and there are many commercially available products. exist. In oral compositions, there is a demand for a feeling of warmth and coolness that can be maintained for a long time after use and strengthened in terms of feeling of use and effect. However, many of the ingredients that give a feeling of warmth and coolness are irritating, and if the amount of these ingredients is increased in order to increase the effect of imparting a feeling of warmth and coolness, stimulation to the oral mucosa will occur, and use I could feel worse.
Therefore, conventionally, by adding baking soda and sodium chloride together with peppermint oil etc., pain in the oral cavity is reduced and a refreshing feeling is given (Patent Document 1; Japanese Patent Application Laid-Open No. 2002-212041), and xylitol is added. It has been proposed to reduce the stimulation of the l-menthol-containing liquid oral composition, which is enhanced by the addition of ethanol at a high concentration (Patent Document 2; Japanese Patent Application Laid-Open No. 2000-178152). A strange taste peculiar to the additive component was generated, and the flavor was sometimes impaired.

By the way, phospholipids and lysophospholipids contained in soybeans, egg yolks, etc. have a strong emulsifying effect, so they are used in a wide range of products such as foods and cosmetics, and are also used as surfactants in oral compositions. It is also known that it can be applied as an antibacterial agent and is effective for preventing or improving oropharyngeal disease and periodontal disease (Patent Document 3; Patent No. 2794072, Patent Document 4; Patent No. 3407206, Patent Document 5; JP-A-2014-88333), it has been proposed that acidic phospholipids or lyso forms thereof can be applied as bitterness reducing agents (Patent Document 6; Patent No. 2717509), but phospholipids and lysophospholipids are It had a peculiar off-taste, which sometimes led to an unpleasant flavor.

Japanese Patent Application Laid-Open No. 2002-212041 JP-A-2000-178152 Japanese Patent No. 2794072 Japanese Patent No. 3407206 JP 2014-88333 A Japanese Patent No. 2717509

The present invention has been made in view of the above circumstances, and an object of the present invention is to provide an oral composition that reduces irritation to the oral mucosa and provides a high feeling of warmth and/or coolness that persists after use. .

The present inventors have made intensive studies to achieve the above objects, and found that when a lysophospholipid is added to an oral composition containing a specific sensation-imparting component that imparts warmth and coolness, a warm sensation and coolness can be obtained. It was found that the effect of imparting feeling is improved, the stimulation to the oral mucosa is reduced, the high feeling of warmth and coolness is maintained even after use, and the unique and unpleasant off-taste derived from lysophospholipids is suppressed.
That is, according to the present invention, (A) lysophospholipid, (B) (B1) one or more components selected from spiranthol, vanillyl ethyl ether, pepper extract, Japanese pepper extract and capsaicin and / or ( B2) By blending with one or more ingredients selected from spearmint oil, carvone, 1,8-cineol, anethole and isopulegol, irritation to the oral mucosa is reduced, and a high warmth sensation that persists even after use. The inventors have found that it is possible to provide an oral composition that imparts a cooling sensation, and have completed the present invention.

In the present invention, by combining the components (A) and (B), particularly in liquid or solid oral compositions, the persistence of warm and cool sensations is remarkably improved, and time elapses after use in the oral cavity. However, it was possible to give a high feeling of warmth and/or coolness. In this case, in order to maintain the warmth and coolness of the oral composition, adding a warming sensation imparting component such as spiranthol or a cooling sensation imparting component such as spearmint oil and increasing the blending amount of these components may cause irritation. On the other hand, phospholipids and lysophospholipids were not found to have the effect of imparting a feeling of warmth or coolness, and they had a peculiar off-taste, which could lead to an unpleasant flavor. However, in the present invention, when the components (A) and (B) are combined, they act synergistically, and the component (A) unexpectedly improves the function of the component (B) to impart warmth and coolness. This has the effect of moderately reducing irritation to the oral mucosa while imparting a high warm feeling and / or refreshing feeling that lasts even after use, and the unpleasant off-taste due to the component (A) It was also possible to suppress and give a pleasant feeling of use.
The action and effect of the present invention were inferior when the component (A) was absent even when the component (B) was contained, and were inferior even when a phospholipid such as phosphatidylcholine was contained instead of the component (A).
As shown in Comparative Examples below, even if the oral cavity composition contains component (B1) or component (B2) as component (B), if component (A) is not added, the sensation of warmth or coolness is not felt. The durability is poor (Comparative Examples 1 and 3 in Tables 1 and 3), and if the component (B) is not blended, the warmth or coolness will not last long even if the component (A) is blended. It was bad (Comparative Examples 2 and 4 in Tables 1 and 3). On the other hand, the oral composition containing the component (A) and the component (B1) or (B2) shown in the examples has an excellent long-lasting feeling of warmth or coolness and is non-irritating to the oral mucosa. The taste was reduced and hardly felt, and the absence of offensive taste was excellent, and almost no offensive taste was felt.

Accordingly, the present invention provides the following oral compositions.
[1]
(A) a lysophospholipid;
(B) (B1) one or more ingredients selected from spiranthol, vanillyl ethyl ether, pepper extract, Japanese pepper extract and capsaicin and/or (B2) spearmint oil, carvone, 1,8-cineol, anethole and and one or more ingredients selected from isopulegol.
[2]
The oral cavity composition according to [1], wherein the mass ratio of (A)/(B1) is 0.1 to 20,000 when it contains component (B1) as component (B).
[3]
The oral cavity composition according to [1], wherein (A)/(B2) is 0.04 to 400 as a mass ratio when it contains component (B2) as component (B).
[4]
(A) the lysophospholipid is one or more selected from lysophosphatidic acid, lysophosphatidylcholine, lysophosphatidylethanolamine, lysophosphatidylserine, lysophosphatidylinositol and salts thereof [1] to [3] oral composition.
[5]
(A) The oral composition according to [4], wherein the lysophospholipid is lysophosphatidylcholine.
[6]
The oral cavity composition according to any one of [1] to [5], wherein the component (B1) is spiranthol and the content thereof is 0.0001 to 0.05% by mass.
[7]
The oral composition according to any one of [1] to [6], wherein the component (B2) is carvone and the content thereof is 0.01 to 5% by mass.
[8]
The oral cavity composition according to any one of [1] to [7], wherein the content of component (A) is 0.02 to 10% by mass.
[9]
The oral composition according to any one of [1] to [8], further comprising (C) 0.01 to 1% by mass of a high-intensity sweetener.
[10]
(C) The oral composition according to [9], wherein the high-intensity sweetener is one or more selected from aspartame, acesulfame potassium, saccharin and saccharin salts.
[11]
The oral composition according to any one of [1] to [10], further comprising (D) a nonionic surfactant.
[12]
The oral composition according to any one of [1] to [11], which is a liquid or solid formulation.
[13]
The oral composition according to [12], which is a mouthwash, mouth freshener or tablet.

ADVANTAGE OF THE INVENTION According to this invention, the composition for oral cavity which reduces irritation|stimulation to an oral mucous membrane and gives a high warm feeling and/or cool feeling which persists after use can be provided.

The present invention will be described in further detail below. The oral composition of the present invention comprises (A) lysophospholipid and (B) (B1) one or more components selected from spiranthol, vanillyl ethyl ether, pepper extract, Japanese pepper extract and capsaicin and/or (B2) and one or more components selected from spearmint oil, carvone, 1,8-cineol, anethole and isopulegol.
In the present invention, the above components (A) and (B1) are active ingredients for imparting warmth, and a combined system of both components can be blended into the oral cavity composition as an agent for imparting warmth. In addition, the above components (A) and (B2) are active ingredients for imparting a refreshing sensation, and a combined system of both components can be blended into the oral cavity composition as a refreshing sensation imparting agent.

(A) The lysophospholipid has the effect of reducing the stimulation of the oral mucosa by the component (B), increasing the effect of imparting a warm sensation and/or a cool sensation, and improving the sustainability of these sensations.
(A) As the lysophospholipid, a compound represented by the following structural formula (1) or a salt thereof can be used.

（式（１）中、Ｒ¹及びＲ²は、いずれか一方が－ＯＨ、他方が－ＯＣＯＲ（Ｒは、炭素数１１～２３の飽和又は不飽和の直鎖状又は分岐鎖状の炭化水素基）であり、Ｘ¹は－Ｈ、－Ｃ₂Ｈ₄Ｎ⁺（ＣＨ₃）₃、－Ｃ₂Ｈ₃（Ｎ⁺Ｈ₃）ＣＯＯＨ、－Ｃ₂Ｈ₄Ｎ⁺Ｈ₃、－Ｃ₆Ｈ₆（ＯＨ）₅、又は－Ｃ₂Ｈ₃（ＯＨ）ＣＨ₂（ＯＨ）である。）

(In the formula (1), one of R ¹ and R ² is —OH and the other is —OCOR (R is a saturated or unsaturated linear or branched hydrocarbon having 11 to 23 carbon atoms) group) and X ¹ is —H, —C ₂ H ₄ N ⁺ (CH ₃ ) ₃ , —C ₂ H ₃ (N ⁺ H ₃ )COOH, —C ₂ H ₄ N ⁺ H ₃ , —C ₆ H ₆ (OH) ₅ or —C ₂ H ₃ (OH)CH ₂ (OH).)

In —OCOR in the above formula (1), R is a saturated or unsaturated linear or branched hydrocarbon group having 11 to 23 carbon atoms, preferably 15 to 21 carbon atoms. Specific examples of —OCOR include lauric acid residue (CH ₃ (CH ₂ ) ₁₀ COO—), myristic acid residue (CH ₃ (CH ₂ ) ₁₂ COO—), palmitic acid residue (CH ₃ (CH ₂ ) ₁₄ COO-), stearic acid residue (CH ₃ (CH ₂ ) ₁₆ COO-), arachidic acid residue (CH ₃ (CH ₂ ) ₁₈ COO-), behenic acid residue (CH ₃ (CH ₂ ) ₂₀ COO-), lignoceric acid residue (CH ₃ (CH ₂ ) ₂₂ COO-), palmitoleic acid residue (CH ₃ (CH ₂ ) ₅ CH=CH(CH ₂ ) ₇ COO-), oleic acid residue (CH ₃ (CH ₂ ) ₇ CH=CH(CH ₂ ) ₇ COO-), linoleic acid residue (CH ₃ (CH ₂ ) ₄ (CH=CHCH ₂ ) ₂ (CH ₂ ) ₆ COO-), γ-linolenic acid residue group ( _CH3 ( _CH2 ) ₄ (CH= _CHCH2 ) ₃ (CH2) _3COO- ), α-linolenic acid residue ( _CH3 ( _{CH2 )} (CH= _CHCH2 ) ₃ ( _CH2 ) _6COO -), erucic acid residue ( _CH3 ( _{CH2 ) 7CH} =CH( _CH2 ) _11COO- ), eicosapentaenoic acid residue ( _CH3CH2 (CH= _CHCH2 ) ₅ ( _CH2 ) _2COO -), docosahexaenoic acid residue (CH ₃ CH ₂ (CH=CHCH ₂ ) ₆ CH ₂ COO-), especially palmitic acid residue (CH ₃ (CH ₂ ) ₁₄ COO-), stearic acid residue ( _CH3 ( _CH2 ) _16COO- ), oleic acid residue ( _CH3 ( _CH2 ) _7CH =CH( _CH2 ) _7COO- ), linoleic acid residue ( _CH3 ( _CH2 ) ₄ (CH= CHCH ₂ ) ₂ (CH ₂ ) ₆ COO-) is preferred.

As the compound represented by the above formula (1), specifically ^, lysophosphatidic acid or a derivative ^thereof is preferable _. H ₄ N ⁺ (CH ₃ ) ₃ ), lysophosphatidylserine (LPS, X ¹ ; -C ₂ H ₃ (N ⁺ H ₃ )COOH), lysophosphatidylethanolamine (LPE, X ¹ ; -C ₂ H ₄ N ⁺ H ₃ ), lysophosphatidylinositol (LPI, X ¹ ; -C ₆ H ₆ (OH) ₅ ), lysophosphatidylglycerin (LPG, X ¹ ; -C ₂ H ₃ (OH)CH ₂ (OH)), etc. mentioned. These may be used singly or in combination of two or more. Lysophosphatidic acid (LPA), lysophosphatidylcholine (LPC), lysophosphatidylethanolamine (LPE), lysophosphatidylserine (LPS), lysophosphatidylinositol (LPI), especially lysophosphatidic acid (LPA), lysophosphatidylcholine (LPC), among others , lysophosphatidylethanolamine (LPE), further lysophosphatidylcholine (LPC), lysophosphatidylethanolamine (LPE), especially lysophosphatidylcholine (LPC), reduce irritation to the oral mucosa and maintain warm and / or cool sensation It is preferable in terms of improvement.
The above compound may be a salt, and examples of the salt include alkali metal salts such as sodium salts and ammonium salts.

In the present invention, the method for producing lysophospholipids is not particularly limited. For example, by enzymatic hydrolysis of the ester bond in the acyl group of lecithin (phospholipid), it can usually be obtained as a phospholipid mixture. .
Furthermore, as the lysophospholipid, a mixture containing unreacted phospholipid that has not been enzymatically decomposed can be used. The lysophospholipid content is preferably high, and when the above mixture is used as (A) the lysophospholipid, the lysophospholipid content is preferably 15% (mass%, hereinafter the same) or more, particularly 20% or more. Lysophospholipid only (100% product) may be used.

(A) As the lysophospholipid, commercially available products such as those manufactured by Avanti Polar Lipid Co., Ltd. and those manufactured by Sigma-Aldrich Co., Ltd. can be used. In addition, egg yolk lysolecithin LPL-1, egg yolk lecithin LPL-20W, egg yolk lecithin LPL-20S manufactured by Kewpie, and SLP-white lyso, SLP-LPC70, SLP-white lyso H, SLP-LPC70H, H manufactured by Tsuji Oil Co., Ltd. . A commercially available product such as LIPOID R LPC20 manufactured by Holstein can also be used.

(A) The content of lysophospholipid is preferably 0.02 to 10%, more preferably 0.05 to 8%, and still more preferably 0.05 to 5% of the total composition. When the blending amount is 0.02% or more, the effect of reducing stimulation of oral mucosa and the effect of improving durability of warm and/or cool feeling can be sufficiently obtained. If it is 10% or less, the offensive taste due to itself can be sufficiently suppressed.

The (B) component is the following (B1) component and/or (B2) component. The component (B1) has a warming effect, and the component (B2) has a refreshing effect, and these components have an irritating property to the oral mucosa.
(B1) component: one or more selected from spiranthol, vanillyl ethyl ether, pepper extract, Japanese pepper extract and capsaicin (B2) component: spearmint oil, carvone, 1,8-cineole, anethole and isopulegol As the component (B), a substance selected from the above components (B1) or a substance selected from the components (B2) can be used. can also be used in combination with the substance of

As the component (B1), spiranthol, Japanese pepper extract, pepper extract, and capsaicin are particularly preferred, and spiranthol is more preferred, from the viewpoints of persisting warmth and reducing irritation. Among the components (B1), spiranthol has a relatively strong stimulus, but in the present invention, by using the component (A) in combination, even if spiranthol is used as the component (B1), the feeling of warmth can be maintained. It is excellent in the effect of reducing sexuality and irritation of oral mucosa, suppresses offensive taste, and has excellent effects.
Component (B2) is preferably spearmint oil, carvone, 1,8-cineol, or anethole, more preferably carvone, from the standpoints of long-lasting coolness and reduced irritation. Among the components (B2), carvone has a relatively low cooling sensation persistence. It has excellent long-lasting sensation and effect of reducing irritation of oral mucosa, suppresses offensive taste, and has excellent action and effect.

Component (B) may be obtained by extracting a raw material plant by a known method under normal extraction conditions. Specifically, solvent extraction is carried out using a polar solvent, a non-polar solvent, or a mixed solvent of a polar solvent and a non-polar solvent, which is pulverized and powdered from raw materials, especially pericarp, fruits, leaves and stems, Alternatively, it can be obtained by steam distillation, supercritical extraction, or pressing. Examples of the extraction solvent include polar solvents such as water, ethyl ether, ethylene chloride, dioxane, acetone, ethanol, methanol, ethyl acetate, propylene glycol, butylene glycol, and glycerin, or n-hexane, petroleum ether, ligroin, and cyclohexane. , carbon tetrachloride, chloroform, dichloromethane, 1,2-dichloroethane, toluene, benzene, or a mixed solvent thereof.
Preferred extraction solvents are water, lower monohydric alcohols having 1 to 5 carbon atoms (especially methanol, ethanol, propanol, isopropanol, etc.), glycols (especially propylene glycol, butylene glycol, etc.), or mixed solvents thereof. The mixed solvent preferably contains water and a lower monohydric alcohol or glycol at a mixing ratio of 10:90 to 90:10 (mass ratio). The extraction solvent may be water only.
Component (B) can be used as a raw material in liquid or solid form. Liquid formulations are preferably liquid formulations, and solid formulations are preferably solid formulations, particularly powders.
The method for solidification is not particularly limited, and for example, a liquid is prepared by adding emulsifying excipients such as gum arabic, gelatin, casein, modified starch, and dextrin, glycerin fatty acid esters, sucrose fatty acid esters, and the like. An emulsifier can be used to form an emulsified liquid, which can then be solidified by known methods such as spray drying, hot air drying, freeze drying, and vacuum drying. It can also be made solid by simply adsorbing it to an excipient such as dextrin. Further, it can be pulverized, fractionated, or the like as necessary to form a powder or granules.
(B) component can also use a commercial item, and specifically, the product of Takasago International Corporation, Ogawa International Corporation, etc. can be used.

The blending amount of component (B) can be adjusted according to the substance used.
When component (B1) is used as component (B), the blending amount (pure amount excluding solvent, etc., hereinafter the same) is preferably within the following range.
When blending spiranthol, vanillyl ethyl ether, capsaicin, the blending amount thereof is 0.0001 to 0.05%, particularly 0.0003 to 0.03%, particularly 0.0005 to 0.03% of the total composition. % is preferred.
When blending pepper extracts and Japanese pepper extracts, the blending amount thereof is 0.001 to 1%, particularly 0.01 to 0.5%, particularly 0.05 to 0.3% of the total composition. preferable.
When the amount of the component (B1) is within the above range, the irritation to the oral mucosa can be sufficiently reduced, and the offensive taste of the component (A) can be sufficiently suppressed.
Further, when component (B2) is used as component (B), its blending amount (pure amount excluding solvent etc., hereinafter the same) is 0.01 to 5%, particularly 0.025 to 1% of the total composition. %, especially 0.05 to 1%.
When the amount of component (B2) is within the above range, irritation to the oral mucosa can be sufficiently reduced, and offensive taste derived from component (A) can be sufficiently suppressed.

In the present invention, it is preferable to use the component (A) and the component (B) ((B1) and/or (B2)) together in an appropriate ratio, and the ratio of these components (A)/( B1) and (A)/(B2) are preferably within the following ranges.
When component (B1) is used as component (B), (A)/(B1), which indicates the quantitative ratio between component (A) and component (B1), is preferably 0.1 to 20,000 as a mass ratio, More preferably 0.25 to 10,000.
Furthermore, when the component (B1) is selected from spiranthol, vanillyl ethyl ether, and capsaicin, (A)/(B1), which indicates the quantitative ratio with the component (B1), is 1 to 20,000 as a mass ratio. is preferred, and more preferably 1.5 to 10,000.
When the component (B1) is selected from Japanese pepper extract and pepper extract, (A)/(B1), which indicates the quantitative ratio with the component (B1), is 0.1 to 2 as a mass ratio. ,000, more preferably 0.25-500.
Further, when using the (B2) component as the (B) component, (A)/(B2), which indicates the quantitative ratio between the (A) component and the (B2) component, is preferably 0.04 to 400 as a mass ratio, More preferably from 0.1 to 100.
When the mass ratio of (A)/(B1) and the mass ratio of (A)/(B2) are within the above ranges, the irritation to the oral mucosa is further reduced, and the warm and/or cool feeling is maintained. Further, the bad taste derived from the component (A) can be suppressed more sufficiently.

The composition for oral cavity of the present invention may further contain (C) a high-intensity sweetener. By blending the component (C) together with the components (A) and (B), the effect of reducing irritation to the oral mucosa can be further improved, and the effect of suppressing the offensive taste derived from the component (A) can be further improved, resulting in better use. you can get a feel.
(C) A sweetener having a relative sweetness of 100 or more can be used as the high-intensity sweetener.
Here, the relative sweetness is the relative sweetness when the sweetness of sucrose (sugar) is 1.0. Information site, https://www.e-healthnet.mhlw.go.jp) describes the usage of substitute sweeteners as relative sweetness of substitute sweeteners to sucrose (same below).

Component (C) specifically includes aspartame (relative sweetness: 100 to 200), acesulfame potassium (relative sweetness: 200), saccharin (relative sweetness: 400 to 500), saccharin salts (saccharin sodium, etc., relative sweetness degree; 400 to 500), sucralose (relative sweetness; 600), stevia (relative sweetness; 300), thaumatin (relative sweetness; 2,000 to 3,000), etc., one selected from these Or 2 or more types can be used. Among them, aspartame, acesulfame potassium, and saccharin sodium are preferred.
(C) A component can use a commercial item.

The blending amount of component (C) is preferably 0.01 to 1%, more preferably 0.02 to 0.5% of the total composition. When the amount is 0.01% or more, the effect of reducing stimulation of the oral mucosa is sufficiently improved, and the effect of suppressing offensive taste derived from the component (A) is also sufficiently improved. If it is 1% or less, its own offensive taste is sufficiently suppressed.

The oral composition of the present invention may further contain (D) a nonionic surfactant. In particular, when a liquid preparation such as a mouthwash or mouth freshener is used, it is preferable to incorporate a nonionic surfactant, so that the component (B) can be sufficiently solubilized.
The nonionic surfactant is not particularly limited, but when it is used as a liquid preparation, polyoxyethylene hydrogenated castor oil is preferable from the viewpoint of stimulation to the oral mucosa and taste, and especially ethylene oxide (EO). Polyoxyethylene hydrogenated castor oil with an average added mole number of 60 to 100 is preferred. In the case of solid preparations, sucrose fatty acid esters, polyglycerin fatty acid esters, and sorbitan fatty acid esters are preferred, and sucrose fatty acid esters are particularly preferred, from the viewpoint of stimulation to the oral mucosa and taste. Commercially available nonionic surfactants can be used.
The content of the nonionic surfactant is preferably 0.05-2%, particularly 0.1-1%, of the total composition.

The shape and dosage form of the oral composition of the present invention are not particularly limited. It can be prepared in the form of a paste, gel, cream, etc.), but can be used in any dosage form.
Liquid preparations include, for example, mouth washes, mouth fresheners, beverages, and the like.
Examples of solid formulations include tablets (plain tablets, sugar-coated tablets, coated tablets, orally disintegrating tablets, chewable tablets, effervescent tablets, etc.), particulates (powder, granules, etc.), capsules, films, pills, Troches, sheets, candies, gummies, chewing gums and the like can be mentioned, but tablets are preferred. As for these shapes, for example, tablet shape, size, etc., a usual shape can be adopted according to the dosage form.
Here, the "oral composition" is "mainly intended to be used in the oral cavity", and is (i) ingestible and (ii) discharged from the oral cavity after use. things are mentioned. Specifically, (i) ingestible solid preparations include tablets, granules, capsules, films, pills, troches, sheets, candies, gummies, and the like, which are used in the oral cavity. It can be applied by licking inside and chewing if necessary. Liquid formulations include beverages and the like, and can be drunk. (ii) Solid preparations that are discharged from the oral cavity after use include mouthwash tablets, mouthwash particulates, chewing gum, etc. These are, for example, dissolved in water at the time of use to prepare liquid preparations. It can also be applied intraorally with Liquid formulations include mouth washes, mouth fresheners, and the like. These are discarded after use. In the present invention, either (i) or (ii) may be used.

In the present invention, liquid or solid preparations, especially mouth washes, mouth fresheners, or tablets are preferable from the viewpoint of the effect of improving the persistence of warm and/or cool sensation, the effect of reducing stimulation of oral mucosa, and the effect of suppressing offensive taste. .

In addition to the above components, the oral composition of the present invention can be prepared by conventional methods by blending known components other than these components as optional components depending on the dosage form and the like.
For liquid preparations, such as mouthwashes, wetting agents, nonionic surfactants as well as other surfactants, solvents, and optionally pH adjusters, sweeteners, flavoring agents, coloring agents, and various other optional agents may be added. Ingredients etc. are blended.
For solid preparations such as tablets, commonly used ingredients such as excipients, binders, lubricants, coating agents, disintegrants, acidulants, sweeteners, flavoring agents, fluidizing agents, coloring agents, etc. can be done. Sugar-free preparations can be prepared without adding sugar, and the tablets do not have to be coated with sugar.

Specific examples of humectants include sugar alcohols such as sorbitol and xylitol, glycerin, propylene glycol, and polyhydric alcohols such as polyethylene glycol having an average molecular weight of 160 to 4000 (average molecular weight according to the Standards for Quasi-drug Ingredients 2006). (The blending amount is usually 5 to 50%).

An anionic surfactant can be used as the surfactant, and examples thereof include alkyl sulfates such as sodium lauryl sulfate and sodium myristyl sulfate, and acyl sarcosinates. The amount of the anionic surfactant is generally 0-10%, particularly 0.01-5%.

Purified water is generally used as the solvent, and about 1 to 40% of ethanol can be added.
Examples of the pH adjuster include citric acid and its salts, malic acid and its salts, hydrogen carbonates, carbonates and the like.

Excipients include, for example, lactose, lactose granules, corn starch, L-cysteine, trehalose, maltitol, sorbitol and the like.

Examples of binders include crystalline cellulose, starch, sucrose, pregelatinized starch, hydroxypropylcellulose, gelatin, gum arabic powder, polyvinylpyrrolidone, pullulan, dextrin, cyclodextrin, methylcellulose, ethylcellulose, hydroxymethylcellulose, hydroxypropylcellulose, hydroxy Propyl methyl cellulose, polyvinyl alcohol, polyethylene glycol and the like.

Lubricants include, for example, calcium stearate, magnesium stearate, sodium stearyl fumarate, sucrose fatty acid ester, light anhydrous silicic acid, talc, fine silicon dioxide and the like.

Coating agents include precipitated calcium carbonate, gelatin, gum arabic, pullulan, carnauba wax, hydroxypropylmethyl phthalate, hydroxyethylcellulose dimethyldiallylammonium chloride and the like. A commercially available premix product such as Opadry (manufactured by Colorcon Japan LLC) may also be used.

Examples of disintegrants include low-substituted hydroxypropylcellulose, hydroxypropyl starch, partially pregelatinized starch, carboxymethylcellulose, salts (sodium salts, calcium salts) and derivatives of carboxymethylcellulose.

Acidulants include citric acid, malic acid, succinic acid, tartaric acid, fumaric acid and the like.
Examples of sweetening agents include dipotassium glycyrrhizinate, glucose-fructose liquid sugar, and starch syrup.

As the flavoring agent, a flavoring agent known as an oral flavoring agent other than the component (B) can be blended.
Fluidizing agents include silicon dioxide, silicic anhydride, titanium oxide, and tricalcium phosphate.

Examples of coloring agents include edible coloring agents, organic pigments and inorganic pigments other than edible coloring agents, and animal and plant extracts. Examples of food colorants include orange essence, caramel, carmine, β-carotene, food blue No. 1, food yellow No. 4, food yellow No. 4 aluminum lake, food yellow No. 5, food red No. 2, food red No. 3, Food Red No. 102 and the like. Examples of organic pigments include sodium copper chlorophyllin, copper chlorophyll, riboflavin, and the like. Examples of inorganic pigments include iron sesquioxide, yellow iron sesquioxide, black iron oxide, zinc oxide, titanium oxide, black iron oxide, brown iron oxide, zinc oxide, gold foil, and medicinal charcoal. Examples of animal and plant extracts include licorice extract, acenyakutannin powder, turmeric extract, and green tea powder. Among these, inorganic pigments are preferable for solid preparations, since they are less likely to fade even after storage and can reduce adhesion to manufacturing machines. Iron sesquioxide, yellow iron sesquioxide, black oxide Inorganic pigments containing iron such as iron as a main component, zinc oxide, and titanium oxide are preferable, iron sesquioxide, yellow iron sesquioxide, zinc oxide, and titanium oxide are more preferable, and iron sesquioxide and yellow iron sesquioxide are even more preferable.
For liquid formulations such as mouthwashes, coloring agents include Blue No. 1, Yellow No. 4, titanium dioxide, and the like.

These optional additive components may be used singly or in combination of two or more, and the amount of each added is a normal amount within a range that does not interfere with the effects of the present invention.

Examples, Comparative Examples, and Formulation Examples are shown below to specifically describe the present invention, but the present invention is not limited to the following Examples. In the following examples, % indicates % by mass unless otherwise specified.

[Examples, Comparative Examples]
Liquid oral compositions (mouthwashes) having compositions shown in Tables 1 to 7 were prepared by the following method.
After each component shown in Tables 1 to 7 was added to a predetermined amount of purified water and dissolved, the mixture was thoroughly stirred using a three-one motor (manufactured by HIDON). The component (B) was mixed with polyoxyethylene (60) hydrogenated castor oil and ethanol, stirred well, and then added to the purified water. Thereafter, purified water was added so that the total amount was 100 g to prepare a mouthwash. A mouthwash of Comparative Example was prepared according to the above method.
The obtained mouthwash was used as a sample, and the feel during use was evaluated by the following method. The results are also shown in Tables 1-7.
The numerical value indicating the blending amount of (A) lysophospholipid is the pure amount of lysophospholipid, and the numerical value indicating the blending amount of component (B) is the pure amount of each component (B) (same below).

<Method for evaluating usability>
Eight subjects held 10 mL of the sample in their mouths and rinsed their mouths for 20 seconds. Each was judged according to the following evaluation criteria. Eight people's average score was calculated and each was judged by the following criteria.
The irritation to the oral mucosa and the absence of offensive taste were evaluated immediately after each sample was used, and the durability of the warm and cool sensations was evaluated after 10 minutes had passed using the sample.

Criteria for evaluation of irritation to oral mucosa;
5 points: no irritation to the oral mucosa 4 points: almost no irritation to the oral mucosa 3 points: slight irritation to the oral mucosa, but acceptable 2 points: irritation to the oral mucosa Sensing irritation 1 point: Sensing strong irritation to the oral mucosa Evaluation criteria for irritation to the oral mucosa ◎: Average score of 4.0 or more and 5.0 or less ○: Average score of 3.0 or more 4. Less than 0 points △: Average score of 2.0 or more and less than 3.0 points ×: Average score of less than 2.0 points

Evaluation criteria for absence of offensive taste 5 points: no offensive taste felt at all 4 points: almost no offensive taste felt 3 points: slightly offensive taste felt but acceptable 2 points: offensive taste felt 1 point: strong offensive taste was felt Criteria for the absence of offensive taste ◎: Average score 4.0 or more and 5.0 or less ○: Average score 3.0 or more and less than 4.0 △: Average score 2.0 or more and 3.0 Less than points ×: Average score less than 2.0 points

Evaluation criteria for durability of cool sensation 5 points: felt a very strong cool sensation 10 minutes after use 4 points: felt a strong cool sensation 10 minutes after use 3 points: felt a cool sensation 10 minutes after use 2 points : Virtually no cooling sensation felt after 10 minutes of use 1 point: No cooling sensation felt at all after 10 minutes of use Judgment criteria for persistence of cooling sensation ◎: Average score of 4.0 to 5.0 points ○: average score of 3.0 or more and less than 4.0 points △: average score of 2.0 or more and less than 3.0 points ×: average score of less than 2.0 points

Evaluation criteria for durability of warmth 5 points: A very strong sensation of warmth was felt 10 minutes after use 4 points: A strong sensation of warmth was felt 10 minutes after use 3 points: A sensation of warmth was felt 10 minutes after use 2 points : Virtually no warmth felt after 10 minutes of use 1 point: No warmth felt at all after 10 minutes of use Judgment criteria for durability of warmth ◎: Average score of 4.0 to 5.0 points ○: average score of 3.0 or more and less than 4.0 points △: average score of 2.0 or more and less than 3.0 points ×: average score of less than 2.0 points

Details of raw materials used are shown below.
(A) Lysophospholipid:
LPC-1 (manufactured by Kewpie Fine Chemicals Co., Ltd., lysophosphatidylcholine
100% content)
(B) component;
(B1) Spilanthol:
Spilanthol (manufactured by Takasago International Corporation, containing 70% Spilanthol)
(B1) vanillyl ethyl ether:
Vanillyl ethyl ether (manufactured by Takasago Perfumery Co., Ltd., vanyl ethyl ether
100% content)
(B1) Japanese pepper extract:
Japanese pepper flavor (manufactured by Ogawa Koryo Co., Ltd., containing 100% Japanese pepper extract)
(B1) pepper extract:
Black pepper oil (Felton Worldwide, pepper extract)
100% content)
(B1) Capsaicin:
Capsaicin (manufactured by Eikodo Honten Co., Ltd., containing 5% capsaicin)
(B2) carvone:
Carvone (manufactured by Shiono Koryo Co., Ltd., containing 100% carvone)
(B2) Spearmint oil:
Spearmint oil (manufactured by Takasago International Corporation, containing 100% spearmint oil)
(B2) 1,8-cineol:
Cineol (manufactured by Takasago Perfumery Co., Ltd., containing 90% 1,8-cineole)
(B2) Anethole:
Anethole (manufactured by Takasago International Corporation, containing 100% anethole)
(C) component;
Aspartame Aspartame (manufactured by Ajinomoto Co., Inc., relative sweetness; 200)
Acesulfame potassium Sunnet Acesulfame K (manufactured by Celanese Japan Co., Ltd., relative sweetness: 200)
Saccharin sodium Saccharin sodium (manufactured by Daito Chemical Industry Co., Ltd., relative sweetness; 500)
(D) component;
Polyoxyethylene (60) hydrogenated castor oil NIKKOL HCO-60 (manufactured by Nikko Chemicals Co., Ltd., average added moles of EO; 60)

A mouthwash having the same composition as in Comparative Example 1 except that vanillyl ethyl ether, pepper extract, Japanese pepper extract or capsaicin was used instead of spiranthol in Comparative Example 1 was evaluated in the same manner. Similar results to Example 1 were obtained.
In addition, a mouthwash having the same composition as in Comparative Example 3 except that spearmint oil, 1,8-cineole, anethole or isopulegol was used instead of carvone in Comparative Example 3 was evaluated in the same manner as in Comparative Example 3. Similar evaluation results were obtained.

In addition, Examples 36 to 41 were superior in both "irritation to oral mucosa" and "absence of offensive taste" compared to those of the same composition except that component (C) was not blended.

A formulation example is shown below.
As the lysophospholipid (A), SLP-white lyso (lysophosphatidylcholine content: about 25%, manufactured by Tsuji Seiso Co., Ltd.) was used ((A) The numerical value indicating the amount of lysophospholipid is the pure amount of lysophosphatidylcholine. is).
(B2) isopulegol is manufactured by Takasago International Corporation (containing 100% isopulegol), (B1) pepper extract is black pepper micron (manufactured by Takasago International Corporation, containing 14% pepper extract), (B2) ) Spearmint oil used spearmint micron 20 (manufactured by Takasago International Corporation, containing 20% spearmint oil) ((B1) pepper extract, (B2) The numerical value indicating the blending amount of spearmint oil is (B1) pepper Extract, (B2) is the pure amount of spearmint oil).
(D) Polyoxyethylene (100) hydrogenated castor oil used was NIKKOL HCO-100 (manufactured by Nikko Chemicals Co., Ltd., average number of moles of EO added: 100).
Except for the above, the same raw materials as in Examples were used.
The fragrance used does not contain the component (B).
Each formulation of the formulation example below was evaluated for irritation to the oral mucosa, absence of offensive taste, and persistence of refreshing sensation by the same method and criteria as above. .

[Prescription Example 1] Mouth freshener A mouth freshener was prepared by stirring the following composition using a three-one motor (manufactured by HIDON). In addition, (B2) component, (D) component, and fragrance|flavor were melt|dissolved in ethanol, and were added. The obtained mouth freshener was filled in a spray container and used by spraying 0.3 mL into the oral cavity by a conventional method.
Composition (A) Lysophospholipid 0.2
(B2) isopulegol 0.01
(C) saccharin sodium 0.01
(D) Polyoxyethylene (100) hydrogenated castor oil 0.3
Glycerin 13
Ethanol 40
Citric acid 0.03
Sodium citrate 0.25
Perfume 0.4
Remainder of purified water
Total 100%

[Prescription Example 2] Mouthwash A mouthwash having the following composition was prepared using Three One Motor (manufactured by HIDON). In addition, (B2) component, (D) component, and fragrance|flavor were melt|dissolved in ethanol, and were added. The obtained mouthwash was used in the manner described in Examples.
Composition (A) Lysophospholipid 0.2
(B2) isopulegol 0.01
(C) saccharin sodium 0.04
(D) Polyoxyethylene (100) hydrogenated castor oil 0.2
Citric acid 0.03
Sodium citrate 0.25
xylitol 2
Glycerin 85% 2
Propylene glycol 2
Ethanol 8
Perfume 0.2
Remainder of purified water
Total 100%

[Prescription Example 3] Tablets With the following composition, tablets were prepared by pressing with a hydraulic single-shot tableting machine (FY-TP-10, manufactured by Fuji Yakuhin Kikai Co., Ltd.) (1 g/tablet, diameter 15 mm). This tablet was used as a sample, and one tablet was licked without being chewed in the oral cavity.
Composition (A) Lysophospholipid 2.0
(B1) pepper extract 0.05
(C) acesulfame potassium 0.1
Fine silicon dioxide 1.0
Calcium stearate 1.0
sorbitol balance
Total 100%

[Prescription Example 4] Tablets With the following composition, tablets were prepared by pressing with a hydraulic single-shot tableting machine (FY-TP-10, manufactured by Fuji Yakuhin Kikai Co., Ltd.) (1 g/tablet, diameter 15 mm). This tablet was used as a sample, and one tablet was licked without being chewed in the oral cavity.
Composition (A) Lysophospholipid 2.0
(B2) spearmint oil 0.1
(C) Aspartame 0.1
Fine silicon dioxide 1.0
Calcium stearate 1.0
sorbitol balance
Total 100%

Claims (9)

(A) lysophosphatidylcholine;
(B) containing one or more components selected from spiranthol, vanillyl ethyl ether, pepper extract, Japanese pepper extract and capsaicin,
The content of component (A) is 0.02 to 10% by mass,
When component (B) is one or more selected from spiranthol, vanillyl ethyl ether and capsaicin, its content is 0.0001 to 0.05% by mass, and (A)/(B) is 0 as a mass ratio. .1 to 20,000;
When the component (B) is one or more selected from pepper extracts and Japanese pepper extracts, its content is 0.001 to 1% by mass, and (A)/(B) is 0.1 as a mass ratio. is ~2,000;
Oral composition. 2. The oral composition according to claim 1 , wherein component (B) is spiranthol. 2. The oral composition according to claim 1, wherein component (B) is one or more selected from vanillyl ethyl ether and capsaicin. 2. The oral composition according to claim 1, wherein the component (B) is one or more selected from a pepper extract and a Japanese pepper extract. The oral composition according to any one of claims 1 to 4, further comprising (C) 0.01 to 1% by mass of a high-intensity sweetener. 6. The oral composition according to claim 5, wherein (C) the high-intensity sweetener is one or more selected from aspartame, acesulfame potassium, saccharin and saccharin salts. The oral composition according to any one of claims 1 to 6, further comprising (D) a nonionic surfactant. The oral composition according to any one of claims 1 to 7, which is a liquid or solid formulation. 9. The oral composition of claim 8, which is a mouthwash, mouth freshener or tablet.